AM211 (AM-211) is a potent, selective and orally bioavailable prostaglandin D2 receptor type 2 (DP2) antagonist with IC50 of 4.9 nM for human DP2.
AM211 inhibits radiolabeled PGD2 binding to mouse, guinea pig, and rat DP2 with IC50 values of 7.8, 4.9, and 10.4 nM, respectively, shows no activity for human TP, IP, DP1, and FP.
AM211 potently antagonizes PGD(2)-stimulated functional responses in relevant human cells, and demonstrates efficacy in animal models of allergic inflammation.
